Dasatinib with Itraconazole Interaction Details
Brand Names Associated with Dasatinib
- Dasatinib
- Sprycel®
Brand Names Associated with Itraconazole
- Itraconazole
- Onmel®
- Sporanox®
- Tolsura®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 31, 2023
Interaction Effect
Increased dasatinib exposure
Interaction Summary
The metabolism of dasatinib, a CYP3A4 substrate, may be inhibited by concomitant administration of itraconazole. Although the interaction between dasatinib and itraconazole has not been studied, an interaction between dasatinib and ketoconazole, another strong CYP3A4 inhibitor, resulted in significant increases in dasatinib exposure. A similar reaction with increases in dasatinib Cmax and AUC can be expected with coadministration of dasatinib and itraconazole. Therefore, concomitant use of dasatinib should be avoided during and for 2 weeks after itraconazole therapy . However, if itraconazole must be administered with dasatinib, then consider reducing the dasatinib dose from 70 mg/day or 100 mg/day to 20 mg daily, or from 140 mg/day to 40 mg daily. For patients on dasatinib 40 mg or 60 mg daily, stop dasatinib until the CYP3A4 inhibitor is discontinued. Monitor patients closely for toxicity. If dasatinib is not tolerated following a dose reduction, then itraconazole must be discontinued or dasatinib must be discontinued until itraconazole treatment is stopped. Once therapy with itraconazole is discontinued, a washout period of approximately 1 week should be allowed before reinitiating dasatinib or increasing the dasatinib dose to the indicated dose .
Severity
Major
Onset
Delayed
Evidence
Theoretical
How To Manage Interaction
Concomitant use of dasatinib, a CYP3A4 substrate, with strong CYP3A4 inhibitors, such as itraconazole, should be avoided during and for 2 weeks after itraconazole therapy. However, if itraconazole must be administered with dasatinib, then consider reducing the dasatinib dose from 70 mg/day or 100 mg/day to 20 mg daily, or from 140 mg/day to 40 mg daily. For patients on dasatinib 40 mg or 60 mg daily, stop dasatinib until the CYP3A4 inhibitor is discontinued. Monitor patients closely for toxicity. If dasatinib is not tolerated following a dose reduction, then either discontinue itraconazole or discontinue dasatinib until itraconazole treatment is stopped. Once therapy with itraconazole is discontinued, allow a washout period of approximately 1 week before reinitiating dasatinib or increasing the dasatinib dose to the indicated dose .
Mechanism Of Interaction
Inhibition of CYP3A4-mediated dasatinib metabolism by itraconazole
Literature Reports
A) Although the interaction between dasatinib and itraconazole has not been studied, an interaction between dasatinib and ketoconazole, a strong CYP3A4 inhibitor, resulted in increased dasatinib plasma concentrations and exposure. Dasatinib Cmax and AUC were increased by 4-fold and 5-fold, respectively, following coadministration of dasatinib 20 mg daily with ketoconazole 200 mg twice daily to patients with solid tumors (n=18) .
Dasatinib Overview
-
Dasatinib is used to treat a certain type of chronic myeloid leukemia (CML; a type of cancer of the white blood cells) as a first treatment and in adults who can no longer benefit from other leukemia medications including imatinib (Gleevec) or in those who cannot take these medications because of side effects. Dasatinib is also used to treat a certain type of chronic CML in children 1 year of age or older. Dasatinib is also used to treat a certain type of acute lymphoblastic leukemia (ALL; a type of cancer of the white blood cells) in adults who can no longer benefit from other leukemia medications or who cannot take these medications because of side effects. It is also used in combination with chemotherapy medications to treat a certain type of ALL in children 1 year of age or older.Dasatinib is in a class of medications called kinase inhibitors. It works by blocking the action of an abnormal protein that signals cancer cells to multiply. This helps stop the spread of cancer cells.
Itraconazole Overview
-
Itraconazole capsules (Sporanox, Tolsura) are used to treat fungal infections in the lungs that can spread throughout the body. Itraconazole capsules (Sporanox) are also used to treat fungal infections of the fingernails and toenails. Itraconazole oral solution (liquid) is used to treat yeast infections of the mouth and throat or of the esophagus (tube that connects the throat to the stomach). Itraconazole is in a class of antifungals called triazoles. It works by slowing the growth of fungi that cause infection.
Return To Our Drug Interaction Homepage
Feedback, Question Or Comment About This Information?
Ask Dr. Brian Staiger, PharmD, our medical editor, directly! He's always more than happy to assist.
Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.